CN103534244B - 氧杂螺[2.5]辛烷衍生物及类似物 - Google Patents

氧杂螺[2.5]辛烷衍生物及类似物 Download PDF

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CN103534244B
CN103534244B CN201280022154.XA CN201280022154A CN103534244B CN 103534244 B CN103534244 B CN 103534244B CN 201280022154 A CN201280022154 A CN 201280022154A CN 103534244 B CN103534244 B CN 103534244B
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mixture
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CN103534244A (zh
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J·E·瓦特
S·查菲
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Larimar Therapeutics Inc
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Zafgen Inc
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    • C07D303/02Compounds containing oxirane rings
    • C07D303/38Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D303/46Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals by amide or nitrile radicals
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    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/336Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
    • AHUMAN NECESSITIES
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    • C07D303/18Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by etherified hydroxyl radicals
    • C07D303/20Ethers with hydroxy compounds containing no oxirane rings
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    • C07D303/12Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms
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    • C07D303/38Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Obesity (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Child & Adolescent Psychology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epoxy Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201280022154.XA 2011-03-08 2012-03-07 氧杂螺[2.5]辛烷衍生物及类似物 Expired - Fee Related CN103534244B (zh)

Applications Claiming Priority (3)

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US201161450301P 2011-03-08 2011-03-08
US61/450,301 2011-03-08
PCT/US2012/028068 WO2012122264A1 (en) 2011-03-08 2012-03-07 Oxaspiro [2.5] octane derivatives and analogs

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CN103534244A CN103534244A (zh) 2014-01-22
CN103534244B true CN103534244B (zh) 2016-10-12

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US (3) US9328082B2 (es)
EP (1) EP2683706B1 (es)
JP (1) JP5876513B2 (es)
KR (1) KR101875988B1 (es)
CN (1) CN103534244B (es)
AU (1) AU2012225531B2 (es)
BR (1) BR112013023056A2 (es)
CA (1) CA2829204C (es)
MX (1) MX342257B (es)
WO (1) WO2012122264A1 (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011085198A1 (en) 2010-01-08 2011-07-14 Zafgen Corporation Metap-2 inhibitor for use in treating benign prostatic hypertrophy (bph)
WO2011127304A2 (en) 2010-04-07 2011-10-13 Zafgen Corporation Methods of treating an overweight subject
CN107141410B (zh) 2010-05-25 2022-12-09 辛德弗雷克斯公司 聚合物缀合的MetAP2抑制剂及其应用的治疗方法
US9895449B2 (en) 2010-05-25 2018-02-20 Syndevrx, Inc. Polymer-conjugated MetAP2 inhibitors, and therapeutic methods of use thereof
KR101875988B1 (ko) 2011-03-08 2018-07-06 자프겐 인크. 옥사스피로[2.5]옥탄 유도체 및 유사체
EP2763671A2 (en) * 2011-10-03 2014-08-13 Zafgen, Inc. Methods of treating age related disorders
BR112014028041A2 (pt) 2012-05-08 2017-06-27 Zafgen Inc tratamento de obesidade hipotalâmica com inibidores de metap2
WO2013169860A1 (en) * 2012-05-09 2013-11-14 Zafgen, Inc. Fumigillol type compounds and methods of making and using same
CA2904353A1 (en) 2013-03-14 2014-09-25 Zafgen, Inc. Methods of treating renal disease and other disorders
AU2014250983B2 (en) 2013-04-10 2019-04-11 Syndevrx, Inc. MetAP2 inhibitors and methods of treating obesity
TW201636342A (zh) * 2014-12-19 2016-10-16 武田藥品工業有限公司 煙黴醇衍生物
CN106432255A (zh) 2015-08-11 2017-02-22 扎夫根公司 烟曲霉素醇螺环化合物和制备和使用其的方法
AR105671A1 (es) 2015-08-11 2017-10-25 Zafgen Inc Compuestos heterocíclicos de fumagillol y sus métodos de elaboración y uso
EP3386956B1 (en) 2015-12-10 2021-07-14 Syndevrx, Inc. Fumagillol derivatives and polymorphs thereof
WO2017123603A1 (en) 2016-01-11 2017-07-20 Syndevrx, Inc. Treatment for tumors driven by metabolic dysfunction
JP2022512826A (ja) 2018-10-26 2022-02-07 シンデブルックス,インコーポレイティド MetAP2阻害剤のバイオマーカーとその応用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6017954A (en) * 1989-08-10 2000-01-25 Children's Medical Center Corp. Method of treating tumors using O-substituted fumagillol derivatives
CN1902215A (zh) * 2003-12-29 2007-01-24 普雷西斯药品公司 甲硫氨酸氨肽酶-2的抑制剂及其用途
WO2010009374A1 (en) * 2008-07-18 2010-01-21 Zafgen, Inc. Methods of treating an overweight or obese subject

Family Cites Families (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5164410A (en) 1988-01-09 1992-11-17 Takeda Chemical Industries, Ltd. Fumagillol derivatives and pharmaceutical compositions thereof
PH26256A (en) 1988-08-12 1992-04-01 Fujisawa Pharmaceutical Co Oxaspiro [2,5] octane derivative
US5180738A (en) 1988-09-01 1993-01-19 Takeda Chemical Industries Fumagillol derivatives and pharmaceutical compositions thereof
DE68927904T2 (de) 1988-09-01 1997-09-04 Takeda Chemical Industries Ltd Fumagillol-Derivate
US5166172A (en) 1988-09-01 1992-11-24 Takeda Chemical Industries, Ltd. Fumagillol derivatives and pharmaceutical compositions thereof
ATE87623T1 (de) 1989-03-06 1993-04-15 Takeda Chemical Industries Ltd 6-epifumagillole, ihre herstellung und ihre verwendung.
US5288722A (en) 1989-03-06 1994-02-22 Takeda Chemical Industries, Ltd. 6-amino-6-desoxyfumagillols, production and use thereof
US5290807A (en) 1989-08-10 1994-03-01 Children's Medical Center Corporation Method for regressing angiogenesis using o-substituted fumagillol derivatives
EP0415294A3 (en) 1989-08-31 1991-06-12 Takeda Chemical Industries, Ltd. Cyclohexanol derivatives, production and use thereof
TW282399B (es) 1990-05-25 1996-08-01 Takeda Pharm Industry Co Ltd
EP0555693B1 (en) 1992-01-30 2001-09-05 Takeda Chemical Industries, Ltd. Method of producing highly watersoluble cyclodextrin complex
ATE153854T1 (de) 1992-12-16 1997-06-15 Takeda Chemical Industries Ltd Stabile pharmazeutische zubereitung mit fumagillolderivaten
KR100286920B1 (ko) 1995-03-27 2001-04-16 디. 꼬쉬 장감염에 대한 약물제조용 푸마길올 및 그의 유도체의 용도
EP0867180A4 (en) 1995-10-11 1999-09-15 Fujisawa Pharmaceutical Co VASCULAR PERMEATION INHIBITOR
EP0799616A1 (en) 1996-04-01 1997-10-08 Takeda Chemical Industries, Ltd. Oral composition comprising a fumagillol derivative
WO1998005293A2 (en) 1996-08-02 1998-02-12 The Children's Medical Center Corporation Method of regulating the female reproductive system through angiogenesis inhibitors
US6207704B1 (en) 1997-06-09 2001-03-27 Massachusetts Institute Of Technology Type 2 methionine aminopeptidase [MetAP2] inhibitors and uses thereof
CA2307792C (en) * 1997-10-31 2007-06-26 Children's Medical Center Corporation Method for regulating size and growth of vascularized normal tissue
KR100357542B1 (ko) 1998-05-15 2002-10-18 주식회사종근당 푸마질롤 유도체 및 그 제조방법
KR100357541B1 (ko) 1998-05-15 2002-10-18 주식회사종근당 5-데메톡시 푸마질롤 유도체 및 그 제조방법
JP2000116337A (ja) 1998-10-09 2000-04-25 Nippon Shokuhin Kako Co Ltd ペットフード
US6383471B1 (en) 1999-04-06 2002-05-07 Lipocine, Inc. Compositions and methods for improved delivery of ionizable hydrophobic therapeutic agents
KR100693771B1 (ko) 1999-04-28 2007-03-12 사노피-아벤티스 도이칠란트 게엠베하 Ppar 수용체 리간드로서의 트리아릴 산 유도체 및 이를 포함하는 약제학적 조성물
US6323228B1 (en) 2000-09-15 2001-11-27 Abbott Laboratories 3-substituted indole angiogenesis inhibitors
US6548477B1 (en) 2000-11-01 2003-04-15 Praecis Pharmaceuticals Inc. Therapeutic agents and methods of use thereof for the modulation of angiogenesis
AU2002239479B2 (en) 2000-11-01 2006-11-09 Praecis Pharmaceuticals Incorporated Peptides as Met-AP2 inhibitors
EP1379241A1 (en) 2001-03-29 2004-01-14 SmithKline Beecham Corporation Compounds and methods
US7087768B2 (en) 2001-09-27 2006-08-08 Equispharm Co., Ltd. Fumagillol derivatives and preparing method thereof
US6803382B2 (en) 2001-11-09 2004-10-12 Galderma Research & Development, S.N.C. Angiogenesis inhibitors and pharmaceutical and cosmetic use thereof
KR100451485B1 (ko) 2002-03-28 2004-10-06 주식회사종근당 푸마질롤 유도체 또는 그 염의 포접 화합물, 및 이를포함하는 약제학적 조성물
US6989392B2 (en) 2002-06-18 2006-01-24 Abbott Laboratories 2-Aminoquinolines as melanin concentrating hormone receptor antagonists
US20040067266A1 (en) 2002-10-07 2004-04-08 Toppo Frank R. Weight loss compound
US20040157836A1 (en) 2002-10-08 2004-08-12 Comess Kenneth M. Sulfonamides having antiangiogenic and anticancer activity
US20040204472A1 (en) 2003-03-04 2004-10-14 Pharmacia Corporation Treatment and prevention of obesity with COX-2 inhibitors alone or in combination with weight-loss agents
KR100552043B1 (ko) * 2004-02-28 2006-02-20 주식회사종근당 푸마질롤 유도체를 포함하는 비만치료용 조성물
MX2007000142A (es) 2004-06-30 2007-03-26 Combinatorx Inc Metodos y reactivos para el tratamiento de desordenes metabolicos.
US20060045865A1 (en) 2004-08-27 2006-03-02 Spherics, Inc. Controlled regional oral delivery
WO2006080591A1 (en) 2005-01-26 2006-08-03 Chong Kun Dang Pharmaceutical Corp. Fumagillol derivatives or method for preparation of fumagillol derivatives, and pharmaceutical compositions comprising the same
FR2886855B1 (fr) 2005-06-08 2009-07-17 Agronomique Inst Nat Rech Utilisation de la fumagilline et de ses derives pour augmenter la biodisponibilite des lactones macrocyliques
US20070078172A1 (en) 2005-06-16 2007-04-05 Jenrin Discovery Mao-b inhibitors useful for treating obesity
EP2170402B1 (en) * 2007-06-26 2015-03-25 Children's Medical Center Corporation Metap-2 inhibitor polymersomes for therapeutic administration
MX2010005857A (es) 2007-11-28 2010-11-22 Mersana Therapeutics Inc Conjugados de analogos de fumagillina biodegradables biocompatibles.
ES2641471T3 (es) 2008-10-06 2017-11-10 The Johns Hopkins University Compuestos de quinolina como inhibidores de la angiogénesis, metionina aminopeptidasa humana, y SirT1, y procedimientos de tratamiento de trastornos
WO2010065879A2 (en) 2008-12-04 2010-06-10 Zafgen Corporation Methods of treating an overweight or obese subject
US8642650B2 (en) 2008-12-04 2014-02-04 Zafgen, Inc. Methods of treating an overweight or obese subject
US20120004162A1 (en) 2008-12-04 2012-01-05 Vath James E Methods of Treating an Overweight or Obese Subject
US20120010259A1 (en) 2008-12-04 2012-01-12 Vath James E Methods of Treating an Overweight or Obese Subject
JP5890312B2 (ja) 2009-10-09 2016-03-22 ザフゲン,インコーポレイテッド 肥満治療に用いられるスルホン化合物
US20130210821A1 (en) 2010-05-27 2013-08-15 James E. Vath Methods for Treating Obesity
WO2012012642A1 (en) 2010-07-22 2012-01-26 Zafgen Corporation Tricyclic compounds and methds of making and using same
AU2011316550A1 (en) 2010-10-12 2013-05-02 Zafgen, Inc Sulphonamide compounds and methods of making and using same
WO2012074968A1 (en) 2010-11-29 2012-06-07 Zafgen Corporation Methods of reducing risk of hepatobiliary dysfunction during rapid weight loss with metap-2 inhibitors
US20140011870A1 (en) 2010-11-29 2014-01-09 Zafgen, Inc. Methods of Treating Obesity Using an Effective Dose of a METAP-2 Inhibitor
JP2013543899A (ja) 2010-11-29 2013-12-09 ザフゲン,インコーポレイテッド 6−o−(4−ジメチルアミノエトキシ)シンナモイルフマギロールの非連日投与を用いた肥満の治療
BR112013018771A2 (pt) 2011-01-26 2019-09-17 Zafgen Inc compostos de tetrazol e métodos para fazer e usar os mesmos
KR101875988B1 (ko) 2011-03-08 2018-07-06 자프겐 인크. 옥사스피로[2.5]옥탄 유도체 및 유사체
BR112013028534A2 (pt) 2011-05-06 2016-09-06 Zafgen Inc compostos tricíclicos parcialmente saturados e métodos para produção e utilização dos mesmos
US9187494B2 (en) 2011-05-06 2015-11-17 Zafgen, Inc. Aryl-substituted tricyclic sulfonamides as methionyl aminopeptidase 2 modulators
MX343688B (es) 2011-05-06 2016-11-16 Zafgen Inc Compuestos tricíclicos de sulfonamida y pirazolo y métodos para su fabricación y uso.

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6017954A (en) * 1989-08-10 2000-01-25 Children's Medical Center Corp. Method of treating tumors using O-substituted fumagillol derivatives
CN1902215A (zh) * 2003-12-29 2007-01-24 普雷西斯药品公司 甲硫氨酸氨肽酶-2的抑制剂及其用途
WO2010009374A1 (en) * 2008-07-18 2010-01-21 Zafgen, Inc. Methods of treating an overweight or obese subject

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Chemical Modification of Fumagillin.I. 6-O-Acyl,6-O-Sulfonyl,6-O-Alkyl,and 6-O(N-Substituted-carbamoyl)fumagillols;Shogo MARUI,等;《Chemical & Pharmaceutical Bulletin》;19920131;第40卷(第1期);96-101 *
Investigation of novel fumagillin analogues as angiogenesis inhibitors;Hyung-Jung Pyun,等;《Bioorganic & MedicinalChemis try Letters》;20040105;第14卷(第1期);91-94 *
金属离子选择性的甲硫氨酰氨肽酶抑制剂研究进展;崔永梅 等;《生命科学》;20060430;第18卷(第2期);155-160 *

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US20150045427A1 (en) 2015-02-12
CN103534244A (zh) 2014-01-22
WO2012122264A1 (en) 2012-09-13
JP2014507477A (ja) 2014-03-27
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CA2829204C (en) 2019-12-24
BR112013023056A2 (pt) 2018-10-09
EP2683706A1 (en) 2014-01-15
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